JP2019523214A5 - - Google Patents

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Publication number
JP2019523214A5
JP2019523214A5 JP2018557405A JP2018557405A JP2019523214A5 JP 2019523214 A5 JP2019523214 A5 JP 2019523214A5 JP 2018557405 A JP2018557405 A JP 2018557405A JP 2018557405 A JP2018557405 A JP 2018557405A JP 2019523214 A5 JP2019523214 A5 JP 2019523214A5
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JP
Japan
Prior art keywords
ala
drug conjugate
iii
edfyd
bt17bdc
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JP2018557405A
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Japanese (ja)
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JP2019523214A (en
JP6942147B2 (en
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Priority claimed from GBGB1607827.1A external-priority patent/GB201607827D0/en
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Publication of JP2019523214A5 publication Critical patent/JP2019523214A5/ja
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Claims (4)

ＢＴ１７ＢＤＣ−２７
またはＢＴ１７ＢＤＣ−２８
から選択される薬物コンジュゲートであって、二環１７−６９−０７−Ｎ２６８が、−ＡＣ ｉ （Ｄ−Ａｌａ）ＮＥ（１Ｎａｌ）（Ｄ−Ａｌａ）Ｃ ｉｉ ＥＤＦＹＤ（ｔＢｕＧｌｙ）Ｃ ｉｉｉ −ＣＯＮＨ ２ を示し、二環１７−６９−０７−Ｎ２４１が、−（ｂＡｌａ）−Ｓａｒ１０−ＡＣ ｉ （Ｄ−Ａｌａ）ＮＥ（１Ｎａｌ）（Ｄ−Ａｌａ）Ｃ ｉｉ ＥＤＦＹＤ（ｔＢｕＧｌｙ）Ｃ ｉｉｉ −ＣＯＮＨ ２ を示し、前記二環がＣ ｉ 、Ｃ ｉｉ 、およびＣ ｉｉｉ 上で環化されて三置換１，３，５−トリスメチルベンゼン構造がもたらされる、薬物コンジュゲート。 BT17BDC-27
Or BT17BDC-28
A Drug conjugates that will be selected from, bicyclic 17-69-07-N268 is, -AC i (D-Ala) NE (1Nal) (D-Ala) C ii EDFYD (tBuGly) C iii -CONH 2 shows a bicyclic 17-69-07-N241 is - a (bAla) -Sar10-AC i ( D-Ala) NE (1Nal) (D-Ala) C ii EDFYD (tBuGly) C iii -CONH 2 A drug conjugate wherein the bicycle is cyclized on C i , C ii , and C iii to provide a trisubstituted 1,3,5-trismethylbenzene structure. スキームＩにおいて記載されている合成経路を含む、請求項１に記載の薬物コンジュゲートを調製する方法。 Including synthetic route described in Scheme I, a method for preparing a drug conjugate of claim 1. １種もしくは複数の薬学的に許容される添加剤と組み合わせて、請求項１に記載の薬物コンジュゲートを含む医薬組成物。 A pharmaceutical composition comprising the drug conjugate of claim 1 in combination with one or more pharmaceutically acceptable additives. がん、特に、固形腫瘍、例えば、非小細胞肺がんの予防、抑制または処置において使用するための、請求項１に記載の薬物コンジュゲート。 Cancer, in particular solid tumors, for example, preventing non-small cell lung cancer, for use in inhibiting or treating drug conjugate according to claim 1.
JP2018557405A 2016-05-04 2017-05-04 Bicyclic peptide-toxin conjugate specific for MT1-MMP Active JP6942147B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1607827.1 2016-05-04
GBGB1607827.1A GB201607827D0 (en) 2016-05-04 2016-05-04 Bicyclic peptide-toxin conjugates specific for MT1-MMP
PCT/GB2017/051250 WO2017191460A1 (en) 2016-05-04 2017-05-04 Bicyclic peptide-toxin conjugates specific for mt1-mmp

Publications (3)

Publication Number Publication Date
JP2019523214A JP2019523214A (en) 2019-08-22
JP2019523214A5 true JP2019523214A5 (en) 2020-06-18
JP6942147B2 JP6942147B2 (en) 2021-09-29

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JP2018557405A Active JP6942147B2 (en) 2016-05-04 2017-05-04 Bicyclic peptide-toxin conjugate specific for MT1-MMP

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US (1) US10994019B2 (en)
EP (1) EP3452096A1 (en)
JP (1) JP6942147B2 (en)
CN (1) CN109414510B (en)
GB (1) GB201607827D0 (en)
WO (1) WO2017191460A1 (en)

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